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用于提高疏水性药物姜黄素口服生物利用度的壳聚糖微粒。

Chitosan microparticles for oral bioavailability improvement of the hydrophobic drug curcumin.

作者信息

Wan Shuxin, Sun Yingqian, Sun Li, Tan Fengping

机构信息

School of Pharmaceutical Science and Technology, Tianjin University, Tianjin, China.

出版信息

Pharmazie. 2012 Jun;67(6):525-8.

Abstract

The aim of this study was to assess the feasibility of microparticles for dissolution enhancement and oral bioavailability of curcumin (Cur). Microparticles were prepared by the ionic crosslinking interaction with the use of tripolyphosphate (TPP) and chitosan (Cs). The physicochemical characteristics of microparticles were investigated. The in vivo performance was assessed by a pharmacokinetic study. The microparticles had an average diameter of 58.50 microm. Acceptable drug loading and encapsulation efficiency of microparticles were obtained to be 33.5% and 85.2%, respectively. Dissolution of Cur enhanced in the microparticles in comparison with pure drug. Drug release profile of Cur from microparticles fitted the first-order model. Microparticles provided improved pharmacokinetic parameters (Cmax 270.24 ng/ml, T(max) 1.30 h) in rats as compared with pure drug (C(max) 87.06 nglml, Tmax 0.66 h). The AUC value of microparticles was 8.4 fold that of the pure drug. The information from this study suggests that the developed microparticles successfully enhanced dissolution of the poorly water-soluble drug Cur, and eventually, improved its oral bioavailability effectively.

摘要

本研究的目的是评估微粒对姜黄素(Cur)溶出度提高及口服生物利用度的可行性。通过使用三聚磷酸钠(TPP)和壳聚糖(Cs),利用离子交联相互作用制备微粒。对微粒的物理化学特性进行了研究。通过药代动力学研究评估其体内性能。微粒的平均直径为58.50微米。微粒的载药量和包封率分别达到33.5%和85.2%,可以接受。与纯药物相比,Cur在微粒中的溶出度有所提高。Cur从微粒中的药物释放曲线符合一级模型。与纯药物(Cmax 87.06 ng/ml,Tmax 0.66 h)相比,微粒在大鼠体内提供了更好的药代动力学参数(Cmax 270.24 ng/ml,T(max) 1.30 h)。微粒的AUC值是纯药物的8.4倍。本研究所得信息表明,所制备的微粒成功提高了难溶性药物Cur的溶出度,并最终有效改善了其口服生物利用度。

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